| 摘要 |
PCT No. PCT/EP94/00216 Sec. 371 Date Nov. 8, 1996 Sec. 102(e) Date Nov. 8, 1996 PCT Filed Jan. 27, 1994 PCT Pub. No. WO95/20564 PCT Pub. Date Aug. 3, 1995Pharmacologically active leukotriene-B4 derivatives of general formula I, <IMAGE> (I) are described, in which R1 represents CH2OH, CH3, CF3, COOR4, CONR5R6, or R2 represents H or an organic acid radical with 1-15 C atoms, R3 symbolizes H; C1-C14 alkyl, C3-C10 cycloalkyl optionally substituted singly or multiply; C6-C10 aryl radicals, independently of one another, optionally substituted singly or multiply by halogen, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carbonyl, carboxyl or hydroxy; or a 5- to 6-membered aromatic heterocyclic ring with at least 1 heteroatom, R4 means hydrogen, C1-C10 alkyl, C3-C10 cycloalkyl; C6-C10 aryl radicals optionally substituted by 1-3 halogen, phenyl, C1-C4 alkyl, C1-C4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxy; CH2-CO-(C6-C10) aryl or a 5- to 6-membered ring with at least 1 heteroatom, A symbolizes a trans, trans-CH=CH-CH=CH, a -CH2CH2-CH=CH- or a tetramethylene group, B symbolizes a C1-C10 straight-chain or branched-chain alkylene group, which optionally can be substituted by fluorine or the group <IMAGE> D means a direct bond, oxygen, sulfur, -C 3BOND C-, -CH=CR7, or together with B can also mean a direct bond, R5 and R6 are the same or different, and represent H or C1-C4 alkyl or R6 represents H and R5 represents C1-C15 alkanoyl or R8SO2, and are optionally substituted with OH, R7 means H, C1-C5 alkyl, chlorine, bromine, R8 has the same meaning as R3, n is 2-5, and, if R4 means hydrogen, their salts with physiologically compatible bases and their cyclodextrin clathrates.
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